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1/20 



Q 

m 
m 

m 
m 

m 

Q 
i: 

w 
ul 
O 
u 



^ ^ 2 oo j::) 



CN CO VO \D VO VO NO 
0\ On On OS ^ 0\ 



0\ 



On OO OO CO ^ 



HH OO 

Q -< <; ^ -<t! 

3 n A. p. 2 S 
o 



O f-i <S 
^ ^ ^ r-l 

< ^ <r! ^ < 
Oh 



2/20 



FIGURE 2 



INHIBITOR 


CONCENTRATION 


ASSAY 


COMBINATION INDEX 


CiJIVliJlrl A 1 ivIPi 






90% Inhibition 


50V. Inhibition 


PAI2:2D7 


10:1 


Entry 


0.043 


0.291 




Z. 1 


riision 


0,017 


A A1 n 

o.oiy 




10*1 


rusion 








50:1 


Fusion 


0.158 


0.046 


PA12:PA14 


10:1 


Entry 


0.437 


0.535 




10:1 


Fusion 


0.22 


0.263 


PA14:2D7 


1:1 


Entry 


2.85 


1.85 




1:1 


Fusion 


1.34 


1.74 


PA12:PA11 


1:1 


Entry 


0.707 


0.641 


PA12:RANTES 


1000:1 


Fusion 


0.331 


0.156 


PA14:RANTES 


100:1 


Fusion 


1.6 


1.37 


2D7:RANTES 


100:1 


Fusion 


0.972 


0.962 


PA12:CD4-IgG2 


10:1 


Fusion 


0.3 


0.31 


PA14:CD4.IgG2 


1:1 


Fusion 


0.957 


0.566 


2D7:CD4-IgG2 


1:1 


Fusion 


1.127 


0.302 



3/20 



o 
m 

m 

m 
m 

m 

rr. 

O 

o 

31 

Q 
u 



a 5 



1 § 

2 Is 



3 



II 



s 

° a 

2 « 

? I 

s .a 



o 



to CO 00 
CN ro fNj 

O O O O ^ '-^ 



O O 



*n o 



o\ ^ ^ ^ 



22 

11 



2 



op oj 2 :5 r3 2 
^ :< <j <; ^ S 



Cm Oh 



CLi 0H Pm Ah 



4/20 



FIGURE 4 



M 


D 


Y 


Q 


V 


S 


S 


P 




Y 


D 


I 


N 


Y 


Y 


T 


s 


E 


P 


c 


Q 


K 


I 


N 


K 


Q 


I 


A 


A 


A 


R 

— 




92 




90 


nd 


83 


— 


82 


nd 


46^ 


40 




— 7 
40 


90 


90 


86 


lit 


49^ 




— 7 
45 


7 

44 










92 














( 

118 




78 


nd 


s: — 

'\ 


36 


— 7 
32 


nd 


4 


-2- 




I 

-0- 


^_ — 






too 










57^ 




^4 




m 










36 










nd 


211 






nd 


10 


^ 




+- 
-19- 


«\ 


52 






36 




36 








^55 


-18- 
-f- 


145 


















-0- 


nd 


175 




-1- 


nd 


14 


-8- 




-h- 


101 






94 
















-13- 


133 










,46 






f 


4- 
-0- 


nd 


112 


80 


81 


nd 


40 


4- 

-22- 










/ 


85 














47' 


i 


1*6 
















— 7 
30 
I' 


4— 

T" 


nd 


76 


81 




nd 




-12- 




49 


76 




40" 


86 


— ^ 












'\ 


-1^ 


93 










43 






86 




nd 


85 


88 


89 


nd 




40 






78 


84 


66, 


76 


80 






86 


64^ 




76 




99 








X 








9( 


) 








95 




100 




H 


Y 


A 


A 


A 


Q 


W 


D 


V 


C 


N 


T 


M 


C 


Q 






89 








— ^ 

40 


130 












82 


4)- 

-1 — 








92 










ri8 


If 


115 




96 


86 




tz 






^\ 


— 








27 


81 




IS9 




I3S 


89 




-0— 

4— 








83 








V 


139 




133 




It2 


97 




+^ 








81 










91 


-25- 


78 




60^ 


94 




-10- 


















91 




77 




76 


79 


103 








— 

73v 


79 








63^ 


83 


-23- 


86 




47 


89 


80 


^= 


77 





2D7 

PAS 

PA9 
PA10 
^ PA11 
PA12 
PA14 

2D7 
PAS 
PAS 
^ PA10 

f*l PA11 tX 



PA 12 
PA14 



2D7 

PAS 
PA9 
^ PAID 



170 



175 



180 



185 



190 



PA 14 

2D7 
PAS 
2 PA9 
U PA10 
PA11 
PA12 
PA 14 



R 


s 


Q 


K E 


G 


i 


H 


Y 


T 


c 


S 


s 


H 


F 


p 


Y 


s 




Y 


Q 


F 


W 


K N 


F 


Q 






nr 


V 










0 


83 


95 








80 


92 




— 7 






»'■ 






102 


n 










1 










90 


100 


51 




1 


90 










95 




























93 


tu 








79 
















1? 










— +— 




1 


y 




-f— 
^- 


25 


84 


96 








77 


82 






























i3S 


130 


i 


78 


95 






9 


91 


99 
















92 




=s 












102 


136 






85 








101 


90 




















85 


88 








80 




-^^ 




9 


109 


83 


5\ 




'■7 


y 


93 


88 






79 











265 



270 



275 



Q 


£ 


F 


F 


G 




N 


N 


c 


S 


S 


S 


N 


R 


L 


D 


Q 














77 


— 




— 


\ 


78 


68 


77 






156 




78 










V 






85 







86 


99 






98 
















4- 






St 


\ 


90 


93 






112 




















93 


103 












128 








-lo- 












78 




\ 










166 






p. 












y 


83 




99 


82 


78 






131 




92 


S2 


>2 






so 




92 


106 


90 


98 


V 


78 






112 



76V.- J 00+% 
51%-75% 
16%-50% 
0%-25V. 
nd 



1 



5/20 



FIGURE 5A 




50 too 150 200 250 300 350 400 

Time (seconds) 



6/20 



FIGURE SB 




7/20 



FIGUKE6A 




8/20 



BlGXJItE 6B 




9/20 



FIGURE 6C 

1400 1 




400 



Concentration (nM) 



-♦-b-JRFL:sCD4 
-»-b-sCD4 alone 
-*-b-JRFL alone 
->«-b-LAI:sCD4 



10/20 



FIGURE 6D 




11/20 




12/20 




13/20 



FIGURE 9 



Combination Index 
CD4-IgG2:T-20 Mass Ratio 
Percent 25:1 25:1 



Inhibition 


(low) 


(high) 


5:1 


1:1 


95 


0.32 


0.20 


0.22 


0.50 


90 


0.38 


0.25 


0.27 


0.55 


85 


0.43 


0.29 


0.30 


0.59 


80 


0.47 


0.33 


0.34 


0.62 


75 


0.51 


0.36 


0.37 


0.65 


70 


0.54 


0.39 


0.40 


0.67 


65 


0.58 


0.42 


0.43 


0.70 


60 


0.61 


0.45 


0.45 


0.73 


55 


0.65 


0.48 


0.49 


0.75 


50 


0.69 


0.51 


0.52 


0.78 



14/20 



o 
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m 
m 
m 
m 

2 
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O 



o 



o 

CO o 



i 

O 

1 

o 
e 
o 

U 



o 



o 



C! 

o 



o 

O S 
Q '6 



00 
CI 

o 

I 

s 

o 

o 



o 

C 

■i 

o 
U 

c 
o 



o 



OS 
CN 



O 
m 



o 



ON 



ON 



OS 



o 
o 



d 



ON 



CO 



oo 



CN 



CN 

o 
c5 



o 
d 



o 
On 



00 



CO 



o 


ON 


0^ 










d 


d 



OS 
o 



o 



CO 
CO 



oo 

CN 



O 
O 



to 

CN 
O 



o 



ON 

m 
o 
o 

d 



o 
d 



o 



15/20 



o 

Oft tj 



C8 

S £ 

d 

o 

U 



ON 



CO 



in 
O 



o 



g « 

a 
o 



o 



.2 

S C3 
Hi H 

o 
U 



.S 13 

.Q - 

B 
o 



Si 

0^ 



o 



oo 



o 
m 



oo 



ro O o\ 



S ^ 

vo 



5S 

oi — c-J 



g CN oo 
^ ^ ^ 



»0 

^ ^ 



^. ^ 



o -I 
t-^ m 



^ to 
d d 



00 



in 

as 



O 

0\ 



o 



.2 

2 

a 
o 
-a 
ca 

o 
C 

o 

I 

o 



CO 

;3 



O 



16/20 



P 



S3 
O 

S3 

S s 

o 
es 
o 
U 



O 



o 



a 
o 



s 
o 

o 

o 



o 



a 
o 
U 

s 

o 



S ' 

o 

,-2 



od 



o 



ON 



O 

o 



to 



vo 



o 



OS 



to 



to 
od 



o 



ON 





VO 




o 


O 


o 


m 




ON 












CO 


--^ 


vd 


r-^ 


to 


r- 

oo 


CO 
VD 




O 


O 




m 


vq 




iO 




ON 

rn 


cn 


lO 


o 


o 


o 


o 

On 


o 


o 



o 

d 
o 

I 

o 

o 
u 

s 

o 



CO 

s 

(1> 
o 



G 
O 

in 

o 

Oh 



17/20 



o 

m 
m 
m 
m 
u 
m 

o 
4: 

o 

m 
O 



O 



O 

ai 



o 

pi! 



o 



2^ 



u 
S 

o 
U 



o 



a 

'•S 

a 

o 



a 
.2 

a 

o 
U 

a 

o 



^ a 
S ^ 

o 

U 

ft-t a 



VO 
On 



o 



06 



m 



ON 
00 



o 



CN 



O 



00 
ON 



CN 



m 

CN 



o 



p 
rn 



O 





CN 


ON 


00 


CN 


CN 




1— ( 


0 


0 




0 


tn 


0 




0 




o\ 







18/20 



o 
m 

ill 

m 

m 

m 

S 

Q 
51 
O 



P 

o 



o 



o 
O 

fr4 



C5 
O 

06 



S3 
O 



s 
o 



4> 

e 

o 

U 



.2 

o 
U 



^ .2 

Si a 



oo 



in 



vo 



vo 



vo 
0\ 



OO ^ 



in 
tn 



O 



OO 

od 



in 
O 



iO 

od ^ 



in 



ON 



cn 
o 

o 

CO 



vo 



o 

ON 



o 



19/20 




20/20 



< 

a. 



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a 



CI 

o 
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Q 



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a 

top 

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in " I 'f " I " r 



I 1 1 T I " I T ' 



I I I ( 



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+ 



in 
o 
+ 



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o 



o 
+ 



lui/ssidoo VMH l-AIH